Oxygenative cleavage of an inert CAr–NH2 bond with concomitant 1,2 amine migration in 8-aminoquinoline derivatives is reported in water at room temperature. The reaction is highly atom- and step-economical as both C- and N-containing fragments of the C–N bond cleavage are incorporated into the target molecule and is effected without the need for N-oxide. The reaction is scalable to gram level, and
据报道,在室温下,
水中
8-氨基喹啉衍
生物中惰性C Ar -NH 2键的氧裂解伴随着1,2胺的迁移。该反应在原子和步骤上都是高度经济的,因为C–N键断裂的含C和N片段都掺入了目标分子中,并且不需要N氧化物即可进行。该反应可扩展至克级,并且该产物可用作偶联反应,催化中的
配体和
生物活性化合物的亲电子伴侣。